MSstatsTMT Improves Accuracy of Thermal Proteome Profiling [PDF]
Molecular and Cellular ProteomicsThermal proteome profiling investigates protein-protein, protein-nucleic acid, or protein-drug interactions, and the impact of metabolite binding and post-translational modifications on these interactions. The experiments quantitatively characterize biological samples treated with small molecules versus controls and subjected to timed exposures to ...
Pierre Jean Beltran +2 more
exaly +4 more sources
Network integration of thermal proteome profiling with multi-omics data decodes PARP inhibition [PDF]
Molecular Systems BiologyComplex disease phenotypes often span multiple molecular processes. Functional characterization of these processes can shed light on disease mechanisms and drug effects.
Mira L Burtscher +13 more
doaj +3 more sources
Identifying the Target of an Antiparasitic Compound in Toxoplasma Using Thermal Proteome Profiling. [PDF]
ACS Chem Biol, 2020 Apicomplexan parasites include the causative agents of malaria and toxoplasmosis. Cell-based screens in Toxoplasma previously identified a chemical modulator of calcium signaling (ENH1) that blocked parasite egress from host cells and exhibited potent antiparasitic activity.
Herneisen AL +5 more
europepmc +8 more sources
Thermal Proteome Profiling in Zebrafish Reveals Effects of Napabucasin on Retinoic Acid Metabolism [PDF]
Molecular and Cellular Proteomics, 2021 Thermal proteome profiling (TPP) allows for the unbiased detection of drug-target protein engagements in vivo. Traditionally, 1 cell type is used for TPP studies, with the risk of missing important differentially expressed target proteins. The use of whole organisms would circumvent this problem. Zebrafish embryos are amenable to such an approach. Here,
Simone Lemeer +2 more
exaly +8 more sources
Thermal proteome profiling (TPP) reveals NAMPT as the anti-glioma target of phenanthroindolizidine alkaloid PF403 [PDF]
Acta Pharmaceutica Sinica BGlioma is difficult to treat due to the unique tumor microenvironment and blood–brain barrier. (13aS)-3-Hydroxyl-6,7-dimethoxyphenanthro[9,10-b] indolizidine (PF403), a phenanthroindolizidine alkaloid, has been identified as a promising therapeutic agent
Fangfei Li +8 more
doaj +4 more sources
Thermal proteome profiling of breast cancer cells reveals proteasomal activation by CDK 4/6 inhibitor palbociclib [PDF]
EMBO Journal, 2018 Palbociclib is a CDK4/6 inhibitor approved for metastatic estrogen receptor-positive breast cancer. In addition to G1 cell cycle arrest, palbociclib treatment results in cell senescence, a phenotype that is not readily explained by CDK4/6 inhibition.
Mikael Bjorklund +2 more
exaly +10 more sources
Membrane-mimetic thermal proteome profiling (MM-TPP) toward mapping membrane protein–ligand dynamic interactions [PDF]
eLifeIntegral membrane proteins (IMPs) are central targets for small-molecule therapeutics, yet robust, unbiased, and detergent-free approaches to assess their on- and off-target interactions remain limited.
Rupinder Singh Jandu +6 more
doaj +2 more sources
Thermal proteome profiling of itaconate interactome in macrophages. [PDF]
Chem SciThermal proteome profiling identified interacting proteins of the immunoregulatory metabolite, itaconate, in macrophages. A novel target, mitochondrial branched-chain-amino-acid aminotransferase (BCAT2), was verified to be inhibited by itaconate.
Meng Y +6 more
europepmc +3 more sources
Characterizing protein-protein interactions with thermal proteome profiling. [PDF]
Curr Opin Struct BiolThermal proteome profiling (TPP) is an innovative technique that uses the principle of protein thermal stability to identify potential protein interaction partners. Employing quantitative mass spectrometry, TPP measures protein stability across the proteome, offering a comprehensive snapshot of protein interactions in a single experiment. When studying
Searle BC.
europepmc +3 more sources
Tandem mass tag-based thermal proteome profiling for the discovery of drug-protein interactions in cancer cells [PDF]
STAR Protocols, 2023 Summary: Identification of effector targets is imperative to the characterization of the mechanisms of action of novel small molecules. Here, we describe steps to identify effector drug-protein interactions in lysates derived from cancer cell lines using
Fraser D. Johnson +4 more
doaj +2 more sources